The invention is directed to a method for the production of a drug in a form, which is suitable for oral administration, contains the active ingredient 2-hydroxy-5-methyllaurophenoxime (HMLO) and clearly improves the bioavailability of this active ingredient and thus offers the prerequisites for the optimum treatment of bronchial asthma and of allergic, rheumatic and inflammatory diseases of different origin.
As is well known, there is a relationship between the solubility, the absorption and the bioavailability of a substance. Drugs of very low solubility are frequently also not absorbed very well. In general, it may be expected that problems with respect to the bioavailability will be encountered if the solubility is less than 0.3% (Ritschel, W. A., Angewandte Biopharmazie (Applied Biopharmacy), Wissenschaftliche Verlagsgesellschaft (Scientific Publishing Company) MBH Stuttgart 1953, page 53; Thoma, K. Oesterreich.-Apotheken-Ztg. (Austrian Pharmacy Journal) 32 (1978) 8, page 157).
It is well known that the bioavailability of drugs of low solubility can be varied for example, by a chemical modification of the drug, by changing the molecular size, by creating suitable pH conditions, by selecting a suitable form of administration, by micronizing, by preparing so-called solid dispersions, as well as by using absorption accelerators.
For example, according to W. A. Ritschel (Ritschel, W. A., Angewandte Biopharmazie (Applied Biopharmacy), Wissenschaftliche Verlagsgesellschaft (Scientific Publishing Company) MBH Stuttgart 1973) organic solvents, such as ethanol, fatty alcohols and fatty esters, surface active materials such as nonionic, anionic and cationic surfactants, saponins, enzymes, complexing agents and carbohydrates, such as sorbitol and glucosamine, are used to improve the bioavailability.
The absorption of the drug HMLO, which has a low solubility, has been modified by using solutions and emulsions, which contain, for example, oils, particularly cotton seed oil, peanut oil, cashew nut oil, corn oil, olive oil, castor oil and sesame oil (GDR Patent DD 235 450 A 1). By these means, the bioavailability can be increased. However, such a preparation is unsuitable for a long-term treatment, because not only can such a treatment disadvantageously affect the fat metabolism, but it can also lead to the necessity of terminating the treatment due to the occurrence of diarrhea.
In the same patent, a plurality of additional auxiliary materials is given, which can be used for a formulation, without any proof being presented of the effect on absorption.